JP2008508289A - 大環状βセクレターゼ阻害剤 - Google Patents

大環状βセクレターゼ阻害剤 Download PDF

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Publication number
JP2008508289A
JP2008508289A JP2007523724A JP2007523724A JP2008508289A JP 2008508289 A JP2008508289 A JP 2008508289A JP 2007523724 A JP2007523724 A JP 2007523724A JP 2007523724 A JP2007523724 A JP 2007523724A JP 2008508289 A JP2008508289 A JP 2008508289A
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JP
Japan
Prior art keywords
compound
alkyl
effective amount
compound according
mmol
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Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Pending
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JP2007523724A
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English (en)
Japanese (ja)
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JP2008508289A5 (enExample
Inventor
アンドリュー ダブリュー. スタムフォード,
イン ファン,
グオチン リ,
コーリー オー. ストリックランド,
ヨハネス エイチ. ボイト,
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Merck Sharp and Dohme LLC
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Schering Corp
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Filing date
Publication date
Application filed by Schering Corp filed Critical Schering Corp
Publication of JP2008508289A publication Critical patent/JP2008508289A/ja
Publication of JP2008508289A5 publication Critical patent/JP2008508289A5/ja
Pending legal-status Critical Current

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/06Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms

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  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
JP2007523724A 2004-07-28 2005-07-26 大環状βセクレターゼ阻害剤 Pending JP2008508289A (ja)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US59189904P 2004-07-28 2004-07-28
PCT/US2005/026468 WO2006014944A1 (en) 2004-07-28 2005-07-26 Macrocyclic beta-secretase inhibitors

Publications (2)

Publication Number Publication Date
JP2008508289A true JP2008508289A (ja) 2008-03-21
JP2008508289A5 JP2008508289A5 (enExample) 2008-09-04

Family

ID=35106859

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2007523724A Pending JP2008508289A (ja) 2004-07-28 2005-07-26 大環状βセクレターゼ阻害剤

Country Status (12)

Country Link
US (2) US7652003B2 (enExample)
EP (1) EP1781644B1 (enExample)
JP (1) JP2008508289A (enExample)
CN (1) CN101027297B (enExample)
AR (1) AR050184A1 (enExample)
AT (1) ATE396990T1 (enExample)
CA (1) CA2575340A1 (enExample)
DE (1) DE602005007245D1 (enExample)
ES (1) ES2306200T3 (enExample)
MX (1) MX2007001102A (enExample)
TW (1) TWI297337B (enExample)
WO (1) WO2006014944A1 (enExample)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2008526913A (ja) * 2005-01-13 2008-07-24 ノバルティス アクチエンゲゼルシャフト Bace阻害剤として有用な大環状化合物

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DE10303974A1 (de) 2003-01-31 2004-08-05 Abbott Gmbh & Co. Kg Amyloid-β(1-42)-Oligomere, Verfahren zu deren Herstellung und deren Verwendung
US7592348B2 (en) 2003-12-15 2009-09-22 Schering Corporation Heterocyclic aspartyl protease inhibitors
US7763609B2 (en) 2003-12-15 2010-07-27 Schering Corporation Heterocyclic aspartyl protease inhibitors
US7700603B2 (en) 2003-12-15 2010-04-20 Schering Corporation Heterocyclic aspartyl protease inhibitors
GB0500683D0 (en) 2005-01-13 2005-02-23 Novartis Ag Organic compounds
BRPI0612072A2 (pt) 2005-06-14 2010-10-19 Schering Corp inibidores da aspartil protease
ES2350854T3 (es) * 2005-06-14 2011-01-27 Schering Corporation Inhibidores de aspartil proteasa.
RU2432362C2 (ru) 2005-11-30 2011-10-27 Эбботт Лэборетриз Моноклональные антитела и их применения
EP1954718B1 (en) 2005-11-30 2014-09-03 AbbVie Inc. Anti-a globulomer antibodies, antigen-binding moieties thereof, corresponding hybridomas, nucleic acids, vectors, host cells, methods of producing said antibodies, compositions comprising said antibodies, uses of said antibodies and methods of using said antibodies
WO2007146225A2 (en) 2006-06-12 2007-12-21 Schering Corporation Heterocyclic aspartyl protease inhibitors
KR20090041387A (ko) * 2006-07-20 2009-04-28 노파르티스 아게 마크로시클릭 락탐
CA2667071A1 (en) 2006-10-06 2008-04-17 Merck & Co., Inc. Macrocyclic spiropiperidine beta-secretase inhibitors for the treatment of alzheimer's disease
JP5379692B2 (ja) 2006-11-09 2013-12-25 プロビオドルグ エージー 潰瘍、癌及び他の疾患の治療のためのグルタミニルシクラーゼの阻害薬としての3−ヒドロキシ−1,5−ジヒドロ−ピロール−2−オン誘導体
US8455626B2 (en) 2006-11-30 2013-06-04 Abbott Laboratories Aβ conformer selective anti-aβ globulomer monoclonal antibodies
WO2008065141A1 (en) 2006-11-30 2008-06-05 Probiodrug Ag Novel inhibitors of glutaminyl cyclase
JP2010512389A (ja) 2006-12-12 2010-04-22 シェーリング コーポレイション アスパルチルプロテアーゼ阻害剤
EP2486928A1 (en) 2007-02-27 2012-08-15 Abbott GmbH & Co. KG Method for the treatment of amyloidoses
ZA200905537B (en) 2007-03-01 2010-10-27 Probiodrug Ag New use of glutaminyl cyclase inhibitors
US9656991B2 (en) 2007-04-18 2017-05-23 Probiodrug Ag Inhibitors of glutaminyl cyclase
EP2200990A1 (en) 2007-09-06 2010-06-30 Schering Corporation Gamma secretase modulators
US8487099B2 (en) 2007-11-05 2013-07-16 Merck Sharp & Dohme Corp. Gamma secretase modulators
WO2009076352A1 (en) 2007-12-11 2009-06-18 Schering Corporation Gamma secretase modulators
MX2010011563A (es) 2008-04-22 2010-11-12 Schering Corp Compuestos 2-imino-3-metil pirrolo pirimidinona fenil-sustituidos como inhibidores de enzima de escision de proteina precursora amiloide sitio beta-1, composiciones y su uso.
CN102282145A (zh) 2008-11-13 2011-12-14 先灵公司 γ分泌酶调节剂
US8759337B2 (en) 2008-12-22 2014-06-24 Merck Sharp & Dohme Corp. Gamma secretase modulators
TW201035103A (en) 2008-12-22 2010-10-01 Schering Corp Gamma secretase modulators
US20120245158A1 (en) 2009-06-16 2012-09-27 Xianhai Huang Gamma secretase modulators
EP2443121A2 (en) 2009-06-16 2012-04-25 Schering Corporation Gamma secretase modulators
WO2010147973A1 (en) 2009-06-16 2010-12-23 Schering Corporation Gamma secretase modulators
EP2475428B1 (en) 2009-09-11 2015-07-01 Probiodrug AG Heterocylcic derivatives as inhibitors of glutaminyl cyclase
US8563543B2 (en) 2009-10-08 2013-10-22 Merck Sharp & Dohme Corp. Iminothiadiazine dioxide compounds as bace inhibitors, compositions, and their use
EP2485590B1 (en) 2009-10-08 2015-01-07 Merck Sharp & Dohme Corp. Pentafluorosulfur imino heterocyclic compounds as bace-1 inhibitors, compositions, and their use
UA108363C2 (uk) 2009-10-08 2015-04-27 Похідні імінотіадіазиндіоксиду як інгібітори bace, композиція на їх основі і їх застосування
US8569310B2 (en) 2009-10-08 2013-10-29 Merck Sharp & Dohme Corp. Pentafluorosulfur imino heterocyclic compounds as BACE-1 inhibitors, compositions and their use
JP6026284B2 (ja) 2010-03-03 2016-11-16 プロビオドルグ エージー グルタミニルシクラーゼの阻害剤
NZ602312A (en) 2010-03-10 2014-02-28 Probiodrug Ag Heterocyclic inhibitors of glutaminyl cyclase (qc, ec 2.3.2.5)
WO2011130377A2 (en) 2010-04-15 2011-10-20 Abbott Laboratories Amyloid-beta binding proteins
WO2011131748A2 (en) 2010-04-21 2011-10-27 Probiodrug Ag Novel inhibitors
EP3533803B1 (en) 2010-08-14 2021-10-27 AbbVie Inc. Anti-amyloid-beta antibodies
JP6050264B2 (ja) 2011-03-16 2016-12-21 プロビオドルグ エージー グルタミニルシクラーゼの阻害剤としてのベンゾイミダゾール誘導体
US9221839B2 (en) 2011-04-07 2015-12-29 Merck Sharp & Dohme Corp. C5-C6 oxacyclic-fused thiadiazine dioxide compounds as BACE inhibitors, compositions, and their use
AU2012298983A1 (en) 2011-08-22 2014-02-27 Merck Sharp & Dohme Corp. 2-spiro-substituted iminothiazines and their mono-and dioxides as BACE inhibitors, compositions and their use
CN106902108B (zh) 2012-03-19 2020-07-21 巴克老龄化研究所 App特异性bace抑制剂(asbi)及其用途
WO2014056816A1 (en) 2012-10-10 2014-04-17 F. Hoffmann-La Roche Ag COMBINATION OF AN Aβ ANTIBODY AND A BACE INHIBITOR
US9422277B2 (en) 2012-10-17 2016-08-23 Merck Sharp & Dohme Corp. Tricyclic substituted thiadiazine dioxide compounds as BACE inhibitors, compositions and their use
WO2014062553A1 (en) 2012-10-17 2014-04-24 Merck Sharp & Dohme Corp. Tricyclic substituted thiadiazine dioxide compounds as bace inhibitors, compositions, and their use
EP2956443B1 (en) 2013-02-12 2019-09-25 Buck Institute For Research On Aging Hydantoins that modulate bace-mediated app processing
CN105175488A (zh) * 2015-09-07 2015-12-23 西北农林科技大学 一种具有抗老年痴呆症活性的化合物及其制备方法
AU2018308088B2 (en) 2017-07-25 2025-05-29 Truebinding, Inc. Treating cancer by blocking the interaction of TIM-3 and its ligand
DK3461819T3 (da) 2017-09-29 2020-08-10 Probiodrug Ag Inhibitorer af glutaminylcyklase
CA3127113A1 (en) 2019-01-30 2020-08-06 Dongxu Sun Anti-gal3 antibodies and uses thereof
AU2021278935A1 (en) 2020-05-26 2022-12-08 Truebinding, Inc. Methods of treating inflammatory diseases by blocking Galectin-3

Citations (4)

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WO2002100399A1 (en) * 2001-06-12 2002-12-19 Elan Pharmaceuticals, Inc. Macrocycles useful in the treatment of alzheimer's disease
WO2002100856A1 (en) * 2001-06-12 2002-12-19 Elan Pharmaceuticals, Inc. Macrocycles useful in the treatment of alzheimer's disease
WO2004043916A1 (en) * 2002-11-12 2004-05-27 Merck & Co., Inc. Phenylcarboxamide beta-secretase inhibitors for the treatment of alzheimer's disease
WO2004062625A2 (en) * 2003-01-07 2004-07-29 Merck & Co., Inc. Macrocyclic beta-secretase inhibitors for treatment of alzheimer's disease

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WO2002100856A1 (en) * 2001-06-12 2002-12-19 Elan Pharmaceuticals, Inc. Macrocycles useful in the treatment of alzheimer's disease
WO2004043916A1 (en) * 2002-11-12 2004-05-27 Merck & Co., Inc. Phenylcarboxamide beta-secretase inhibitors for the treatment of alzheimer's disease
WO2004062625A2 (en) * 2003-01-07 2004-07-29 Merck & Co., Inc. Macrocyclic beta-secretase inhibitors for treatment of alzheimer's disease

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2008526913A (ja) * 2005-01-13 2008-07-24 ノバルティス アクチエンゲゼルシャフト Bace阻害剤として有用な大環状化合物

Also Published As

Publication number Publication date
HK1102328A1 (en) 2007-11-16
EP1781644A1 (en) 2007-05-09
ES2306200T3 (es) 2008-11-01
CA2575340A1 (en) 2006-02-09
WO2006014944A1 (en) 2006-02-09
US7652003B2 (en) 2010-01-26
CN101027297A (zh) 2007-08-29
US20100178294A1 (en) 2010-07-15
DE602005007245D1 (enExample) 2008-07-10
US20060040948A1 (en) 2006-02-23
MX2007001102A (es) 2007-04-13
TW200607807A (en) 2006-03-01
US8012953B2 (en) 2011-09-06
AR050184A1 (es) 2006-10-04
TWI297337B (en) 2008-06-01
CN101027297B (zh) 2010-09-08
EP1781644B1 (en) 2008-05-28
ATE396990T1 (de) 2008-06-15

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